Research Abstracts Online
January
2008 - March 2009

University of Minnesota Twin Cities
Medical School
Department of Medicine

PI: Arkadiusz Dudek

Investigations of the Mechanism of Action of a Novel Quinoline, MT477

MT477 is a novel thiopyrano[2,3-c]quinoline that has been identified using molecular topology screening as a potential anticancer drug with a high activity against protein kinase C (PKC) isoforms. The objective of this research is to determine the mechanism of action of MT477 and its activity against human cancer cell lines. MT477 interferes with PKC activity as well as phosphorylation of Ras and ERK1/2 in H226 human lung carcinoma cells. It also induces poly-caspase-dependent apoptosis. MT477 had a dose-dependent (0.006 to 0.2 mM) inhibitory effect on cellular proliferation of H226, MCF-7, U87, LNCaP, A431, and A549 cancer cell lines as determined by in vitro proliferation assays. This study evaluates this novel compound on gene expression in human lung cancer cells.

The researchers perform gene array analysis in order to identify potential other targets for this compound.